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br Introduction Receptor tyrosine kinases RTKs are
2021-03-03

Introduction Receptor tyrosine kinases (RTKs) are critically involved in the development and progression of human cancers and are therefore useful targets for anti-cancer therapies [1]. The Eph receptors represent the largest subfamily of receptor protein kinases and interact with ligands called
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Through an unknown mechanism RING Ubox type
2021-03-03

Through an unknown mechanism, RING/Ubox-type E3 dimers and the N-terminal tail have been shown to function as a modulator of full E3 ubiquitin ligase activity [27]. LRSAM1 promotes a significant enhancement in the formation of the high-molecular-weight products or E3 activity when the RING domain is
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br Concluding remarks and prospective Cardiac
2021-03-03

Concluding remarks and prospective Cardiac proteinopathy, a more common disease condition and more frequent cause of cardiomyocyte decay than previously thought, is largely neglected and no effective therapy exists yet. Protein quality control and protein degradation via autophagy or the ubiquiti
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br Conflicts of interest br Acknowledgements br Introduction
2021-03-03

Conflicts of interest Acknowledgements Introduction Atherosclerosis is the number one cause of death in the United States and among the leading causes of morbidity and mortality globally [1]. Inflammation is critical in all stages of atherosclerosis from the formation of a plaque in the ves
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(R)-baclofen synthesis Besides being the only enzyme E is al
2021-03-03

Besides being the only enzyme, E1 is also the largest and arguably most complex protein encoded by papillomaviruses. As the replicative helicase, E1 plays a central role in the viral life cycle. To do so, E1 engages in multiple protein–protein and protein–nucleic (R)-baclofen synthesis interactions
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br Molecular modeling study Molecular modeling study was
2021-03-03

Molecular modeling study Molecular modeling study was essentially needed to understand and interpret the DHFR inhibitory pattern of this new class of compounds. Computational docking is an algorithm designed to estimate two main terms. The first is to determine the suitable position and the orien
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With regard to the DGATs we have found that the
2021-03-03

With regard to the DGATs, we have found that the majority of algal species encode at least one DGAT1, although it appears to be absent from Ostreococcus and Micromonas, as is the case for yeast, S. cerevisiae. More surprising is the presence of multiple DGAT2 genes in algae, with the exception of C
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In Hevea brasiliensis both the soluble
2021-03-03

In Hevea brasiliensis, both the soluble PPase and the membrane-bound V-PPase are present in the latex; the soluble PPase is in the C-serum (cytosol) of the latex [6] and the V-PPase is on the tonoplast of the lutoid, a special vacuole in the laticifers of rubber trees [7]. The V-PPase on the lutoid
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Imidazo purine diones were another cluster of compounds iden
2021-03-03

1-Imidazo[2,1-]purine-2,4(3,8)-diones were another cluster of compounds identified from the Chembridge screen (). A benzyl group at the R2 position was preferred over a phenyl or 2-phenylpropyl (. and ), and -substitution of the benzyl group increased potency to the nanomolar level ( IC=0.20μM . ).
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Given a disruption of membrane internalization
2021-03-03

Given a disruption of membrane internalization and an increase in synaptic glutamate receptors in CPG2 knockdown neurons, one might expect an increase in dendritic spine size as membrane continues to be inserted into the spines during receptor exocytosis. However, we observed the opposite phenotype,
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Many PIM inhibitors have been reported to date
2021-03-02

Many PIM inhibitors have been reported to date [7], [8], [9] however, none of them has been marketed so far. SGI-1776 is a representative first-generation PIM inhibitor, which had been under clinical trials for leukemia and prostate cancer [10]. While most of the first-generation PIM inhibitors are
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Z-VEID-FMK receptor Targeting the MAPK pathway has
2021-03-02

Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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Although the mechanisms underlying the
2021-03-02

Although the mechanisms underlying the EP4-mediated increase in the frequency of mEPSCs via PGE2 remain unclear, mechanisms similar to those driven by EP2 may be involved because activation of both these receptor subtypes increases the intracellular concentration of cAMP (Nishigaki et al., 1995, Sug
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In the present study it was
2021-03-02

In the present study, it was particularly of interest that intravesical administration of PGE2 evoked ONO-8130-reversible rapid phosphorylation of ERK in the L6 spinal cord. Detection of phosphorylated ERK is now often used as a marker for somatic and visceral nociception, including hydroxylase inhi
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The Acat gene was identified by functional
2021-03-02

The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, cholinesterase inhibitor 1 and 7, with each site containing a distinct promoter: chromosome 1 c
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